SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USE THEREOF Russian patent published in 2013 - IPC C07D401/04 C07D401/14 C07D451/04 C07D451/14 C07D471/14 A61K31/498 A61K31/4985 A61K31/46 A61P25/04 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to substituted quinoxaline-type piperidine compounds of formula or to a pharmaceutically acceptable derivative thereof, wherein: Y₁ represents O; Q is specified in condensed benzo or pyridino; each R₂ is independently specified in: (a) -halogen or -CN; (b) -(C₁-C₆)alkyl; a is an integer specified in 0, 1 or 2; a dash line in a 6-member ring containing a nitrogen atom which is condensed with Q group means the presence or absence of a bond, and when the dash line means the absence of the bond, then R₃, and one R₄ are absent; R₃ is specified in: (a) -H; each R₄ is independently specified in: (a) -H; or (b) - halogen or CN; or (c) -X, -(C₁-C₆)alkyl-X, -(5- or 6-member)heterocyclyl-X or -(5- or 6-member)heterocyclyl-(C₁-C₆)alkyl-X; or (d) -C(=Y)X, -C(=Y)T₃, -C(=Y)YX, - C(=Y)YT₃, -C(-Y)N(T₁)(T₂), -C(=Y)N(R₉)CN, -C(=Y)N(R₉)X, -C(=Y)N(R₉)YH, -C(=Y)N(R₉)YX, -C(=Y)N(R₉)YCH₂X, -C(-Y)N(R₉)YCH₂CH₂X or -C(=Y)N(R₉)S(K))₂T₃; or (e) -N(R₉)X, -N(R₉)-CH₂X, -N(R₉)-CH₂CH₂X, -N(R₉)CH₂N(R₉)C(=N(R₁₂))N(R₁₂)₂, -N(R₉)-CH₂CH₂N(R₉)C(=N(R_I2))N(R₁₂)₂, -N(T₁)(T₂), -N(T₃)C(=Y)T₃, -N(T₃)C(=Y)YT₃, -N(T₃)C(=Y)N(T₁)(T₂), -N(T₃)S(=O)₂T₃ or -N(T₃)S(=O)₂N(T₁)(T₂); X represents: (a) -H, -( C₁-C₆)alkyl, -(C₂-C₆)alkenyl, -(C₁-C₆)alkoxy, -(C₃-C₇)cycloalkyl, -(5- or 6-member)heterocycle or -(7-10-member)bicycloheterocycle each of which is unsubstituted or substituted with 1, 2 or 3 of optionally substituted R₈ groups; or (b) -phenyl, -naphthalenyl, or -(5- or 6-member)heteroaryl each of which is unsubstituted or substituted with 1 or 2 of independently specified in R₇ groups; each Y is independently specified in O; A and B are independently specified in: (a) -H; or (c) A-B together can form a (C₂-C₆)bridge each can optionally contain -HC=CH- or -O- in a (C₂-C₆)bridge; wherein the 6-member ring containing a nitrogen atom which is condensed with Q group can be found in the endo- or exo- configuration in relation to the A-B bridge; or (d) A-B together can form the -CH₂-N(R_a)-CH₂- bridge wherein the 6-member ring containing a nitrogen atom is condensed with Q group, and can be found in the endo- or exo- configuration in relation to the A-B bridge; R_a is specified in -H or -(C₁-C₆)alkyl; Z represents -[(C₁-C₁₀)alkyl optionally substituted with R₁]_h-, wherein h is equal to 0 or 1; each R₁ is independently specified in: (b) -(C₁-C₁₀)alkyl, -(C₂-C₁₀)alkenyl, -(C₂-C₁₀)alkynyl₃ -(C₃-C₇)cycloalkoxy, -(C₆-C₁₄)bicycloalkyl, -(C_8-C₁₀)tricycloalkyl, -(C₅-C₁₀)cycloalkenyl, -(C₇-C₁₄)bicycloalkenyl, -(3-7-member)heterocyclyl each of which is unsubtituted or substituted with 1, 2 or 3 of independently specified in R₈ groups;

or or (d) -phenyl, -naphthalenyl each of which is unsubstituted or substituted with R₇ group; each R₆ is optionally specified in -H; each R₇ is independently specified in -(C₁-C₄)alkyl, -OR₉, -C(halogen)₃, -CH(halogen)₂, -CH₂(halogen), -CN, -halogen, -N(R₉)₂, -C(=O)OR₉; each R₈ is independently specified in -(C₁-C₄alkyl, tetrzolyl, imidazolyl, furanyl, -(C₁-C₆)alkylCOOR₉, -OR₉, -SR₉, -C(halogen)₃, -CH(halogen)₂, -CH₂(halogen), -CN, =O, -halogen, -N(R₉)(C₁-C₆)alkylCOOR₉, -N(R₉)₂, -N(R₉)S(=O)₂R₁₂, -N(R₉)C(=O)R₁₂, -N(R₉)C(=O)OR₁₂, -C(=O)R₉, -C(=O)N(T₁)(T₂), -C(=O)OR₉, -OC(=O)R₉, or -S(=O)₂R₉; each R₉ is independently specified in -H, -(C₁-C₆)alkyl, -(C₃-C₈)cycloalkyl, -phenyl, -benzyl, -(5- to 6-member)heterocycle, -C(halogen)₃; -CH(halogen)₂ or -CH₂(halogen); if h is equal to O, then R₁₁ can be specified in -H, -C(=O)OR₉ or -C(=O)N(R₆)₂ or R₁₁ can be -(C₁-C₄)alkyl; if h is equal to 1, then R₁₁ can be specified in -H; each R₁₂ is independently specified in -H or -(C₁-C₄)alkyl; m is equal to an integer specified in 3, 4, 5, 6, 7, 8 or 9; each e and f is equal to an integer independently specified in 0 or 1, provided 2≤(e+f)≤5; each j and k is equal to an integer independently specified in 0 or 1, provided 1≤(j+k)≤4; each p is equal to an integer independently specified in 0 or 1; each T₁, T₂, and T₃ is independently specified in -H or -(C₁-C₁₀)alkyl which is unsubstituted or substituted with 1, 2 or 3 from independently specified R₈ groups, or T₁ and T₂ together can form 5- to 8-member ring wherein the number of ring atoms contains a nitrogen atom wherein T₁ and T₂ are bound; the above 5- to 8-member ring is unsubstituted or substituted with 1, 2 or 3 from independently specified R₈ groups and optionally any carbon atom in the above 5- to 8-member ring is independently substituted with O or N(R₆); each halogen is independently specified in -F, -CI, -Br or -I.

EFFECT: invention refers to the intermediate compounds of formula

, , for preparing the above compounds of formula (II), compositions containing the above compounds and to a method of treating or preventing a diseased state, such as a pain.

36 cl, 58 ex, 2 tbl